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Compounds, compositions and Methods for modulating CFTR (transmembrane conductance regulator of cystic fibrosis)
专利权人:
PROTEOSTASIS THERAPEUTICS; INC.
发明人:
PARKS, DANIEL,BASTOS, CECILIA M.,MUNOZ, BENITO
申请号:
ARP170100899
公开号:
AR108203A1
申请日:
2017.04.07
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
Claim 1, characterized in that: a compound is selected from N - (2,4 - Di - tert - butyl - 4 - hydroxyphenyl) - 4 - oxo - 1.4 - dihidroquinolin - 3 - carboxamide and a pharmaceutically acceptable Salt thereof,Where at least one carbon Atom is replaced by silicon.Claim 9 wherein: a compound represented by the formula (1) or a pharmaceutically acceptable Salt thereof,Where: x\u00b9 is selected from the group consisting \u2083 (r\u00b3) -, - C (cy\u00b3) \u2083, Hydrogen, halogen, c\u2081\u208b\u2083alquilo optionally substituted with one or more halogens, c\u2083\u208b\u2086cicloalquilo,And heterociclilo monocyclic saturated 4-6 members where c\u2083\u208b\u2086cicloalquilo monocyclic and heterociclilo saturated 4-6 members can be optionally replaced with one, two,Three or more substituents selected independently in each case between r\u00b9\u00b9 X is selected from the group consisting \u2083 if (r\u00b3) and C (cy\u00b3) \u2083 where at least one of x\u00b9 or if (X is r\u00b3) \u2083 R- is selected independently in each case among the group consisting c\u2081\u208b\u2084alquilo, c\u2081\u208b\u2084alcoxi, hydroxyl and phenyl, where c\u2081\u208b\u2084alquilo, c\u2081\u208b\u2084alcoxi,And phenyl can be optionally replaced with one, two,Three or more deuterium Atoms or groups two r\u00b3 along with silicon to form a United ciclosilano which are saturated with 4 - 6 members and selected independently in each case between theGroup consisting of hydrogen and deuterium, and r\u00b9\u00b9 is selected independently in each case among the group consisting of hydrogen, halogen, Hydroxy, cyano,And c\u2081\u208b\u2086alquilo where c\u2081\u208b\u2086alquilo can be optionally substituted by one or more substituents selected independently in each case among the group is Halogen, Hydroxy,And c\u2081\u208b\u2086alcoxi. Claim 16: a Pharmaceutical composition which comprises a compound of any of claims 1 to 15 and a pharmaceutically acceptable excipient.The Method of claim 21: any
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